TABLE 1.
Initial screening of BAs (100 μM) toward various important UGT forms
| Bile Acids | UGT1A1 | UGT1A3 | UGT1A4 | UGT1A6 | UGT1A7 | UGT1A8 | UGT1A9 | UGT1A10 | UGT2B7 | UGT2B15 |
| HDCA | 44.6 ± 0.4*** | 26.1 ± 6.8* | 13.7 ± 0.5** | 95.4 ± 2.1 | 47.8 ± 0.5*** | 84.0 ± 6.1* | 50.4 ± 4.3* | 52.5 ± 0.9*** | 9.5 ± 2.0** | 34.6 ± 0.4*** |
| LCA | 21.1 ± 8.0*** | 16.4 ± 0.5* | 0.0 ± 0.0*** | 19.9 ± 1.3** | 30.0 ± 2.2*** | 64.3 ± 7.1** | 65.2 ± 17.4 | 25.0 ± 0.3*** | 15.7 ± 1.9** | 0.3 ± 0.0*** |
| TCDCA | 17.5 ± 6.7*** | 21.6 ± 1.3* | 27.8 ± 2.1** | 84.6 ± 1.6* | 52.7 ± 3.3*** | 59.1 ± 20.0* | 75.3 ± 1.1* | 41.0 ± 8.2** | 28.1 ± 2.0** | 28.4 ± 1.1*** |
| Taurocholic acid sodium salt hydrate | 62.7 ± 6.1** | 66.7 ± 17.3 | 73.8 ± 1.4 | 105.8 ± 0.4 | 94.1 ± 2.5 | 75.5 ± 8.1* | 94.7 ± 6.2 | 71.9 ± 0.3** | 69.3 ± 7.7* | 70.2 ± 3.9* |
| CDCA | 37.7 ± 8.4** | 47.2 ± 8.0 | 20.2 ± 1.4** | 92.9 ± 2.6 | 47.4 ± 12.7** | 29.2 ± 3.1*** | 74.0 ± 1.2* | 39.9 ± 2.3*** | 15.4 ± 2.1** | 19.8 ± 1.0*** |
| TLCA | 5.4 ± 0.0*** | 3.4 ± 0.4* | 0.0 ± 0.0*** | 52.4 ± 0.2** | 9.1 ± 8.8*** | 24.1 ± 3.5*** | 54.4 ± 7.1* | 14.8 ± 6.8*** | 1.7 ± 0.6** | 5.3 ± 0.0*** |
| UDCA | 27.4 ± 0.4* | 92.8 ± 49.8 | 25.3 ± 0.8** | 85.0 ± 0.9* | 45.7 ± 9.6** | 29.8 ± 3.8*** | 54.5 ± 5.8* | 57.6 ± 1.4*** | 46.2 ± 4.9* | 54.1 ± 1.2** |
| CA | 61.9 ± 0.2** | 135.5 ± 18.8 | 73.0 ± 1.1 | 100.7 ± 1.0 | 103.4 ± 2.8 | 86.1 ± 3.2* | 89.0 ± 3.7 | 74.4 ± 0.5** | 83.2 ± 7.9 | 72.1 ± 0.2** |
| DHCA | 76.4 ± 13.3 | 117.5 ± 30.2 | 80.7 ± 25.3 | 95.0 ± 0.7 | 80.9 ± 1.7** | 87.1 ± 16.0 | 83.0 ± 3.5 | 90.5 ± 2.9* | 81.0 ± 3.1 | 77.7 ± 1.1* |
| DCA | 33.9 ± 2.3*** | 57.8 ± 11.8 | 43.8 ± 21.8* | 90.3 ± 2.5 | 68.0 ± 3.7** | 88.7 ± 32.5 | 67.5 ± 2.6* | 39.1 ± 1.5*** | 45.8 ± 2.2* | 35.4 ± 1.0*** |
| TUDCA | 10.6 ± 0.1*** | 49.1 ± 8.5 | 30.8 ± 4.6** | 76.9 ± 2.4* | 48.8 ± 11.1** | 59.3 ± 0.6*** | 82.9 ± 9.1 | 38.2 ± 13.2** | 26.1 ± 2.3** | 25.3 ± 0.7*** |
| TDCA | 34.1 ± 0.1** | 61.1 ± 8.8 | 41.1 ± 13.3 | 93.4 ± 1.1 | 60.4 ± 2.5*** | 74.7 ± 11.3 | 85.0 ± 0.5 | 50.8 ± 1.0* | 33.4 ± 2.0* | 40.7 ± 1.9*** |
| GCA | 65.4 ± 4.5** | 143.2 ± 44.3 | 54.5 ± 10.3 | 91.6 ± 2.9 | 82.0 ± 15.0 | 80.9 ± 8.7 | 94.0 ± 4.8 | 75.7 ± 3.8** | 48.4 ± 3.5* | 63.4 ± 1.5** |
The values shown are the residual activity, which was calculated using the following equation: % residual activity = (the activity at 100 μM BAs/the control activity at 0 μM BAs) × 100%. *P < 0.05, **P < 0.01, ***P < 0.001, compared with control activity.